Modular Synthesis of Diverse Natural Product-like Macrocycles: Discovery of Hits with Antimycobacterial Activity

Autor: Dow, M, Marchetti, F, Abrahams, KA, Vaz, L, Besra, GS, Warriner, S, Nelson, A

A modular synthetic approach was developed in which variation of the triplets of building blocks used enabled systematic variation of the macrocyclic scaffolds prepared. The approach was demonstrated in the synthesis of 17 diverse natural product-lik

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=core_ac_uk__::1171baa1c2a9257bf20926b79221a828
https://eprints.whiterose.ac.uk/114554/10/Dow_et_al-2017-Chemistry_-_A_European_Journal.pdf

The enzymology of Streptococcus pneumoniae peptidoglycan polymerisation

Autor: Abrahams, Katherine Anne

Bacterial cell survival depends on intact peptidoglycan, an extensive cell wall polymer of alternating N-acetylglucosamine and N-acetylmuramic acid residues, cross-linked by short peptides. Peptidoglycan biosynthesis is a viable and validated antimic

Externí odkaz: http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.570559

DprE2 is a molecular target of the anti-tubercular nitroimidazole compounds pretomanid and delamanid.

Autor: Abrahams KA; Institute of Microbiology and Infection, School of Biosciences, University of Birmingham, Edgbaston, Birmingham, B15 2TT, UK., Batt SM; Institute of Microbiology and Infection, School of Biosciences, University of Birmingham, Edgbaston, Birmingham, B15 2TT, UK., Gurcha SS; Institute of Microbiology and Infection, School of Biosciences, University of Birmingham, Edgbaston, Birmingham, B15 2TT, UK., Veerapen N; Institute of Microbiology and Infection, School of Biosciences, University of Birmingham, Edgbaston, Birmingham, B15 2TT, UK., Bashiri G; Laboratory of Molecular and Microbial Biochemistry, School of Biological Sciences, University of Auckland, 3A Symonds Street, Auckland, 1010, New Zealand., Besra GS; Institute of Microbiology and Infection, School of Biosciences, University of Birmingham, Edgbaston, Birmingham, B15 2TT, UK. g.besra@bham.ac.uk.

Publikováno v: Nature communications [Nat Commun] 2023 Jun 28; Vol. 14 (1), pp. 3828. Date of Electronic Publication: 2023 Jun 28.

GSK2556286 Is a Novel Antitubercular Drug Candidate Effective In Vivo with the Potential To Shorten Tuberculosis Treatment.

Autor: Nuermberger EL; Center for Tuberculosis Research, Division of Infectious Diseases, Johns Hopkins Universitygrid.21107.35grid.471401.7grid.21107.35 School of Medicine, Baltimore, Maryland, USA., Martínez-Martínez MS; Diseases of the Developing World, GlaxoSmithKline R+D Limited, Tres Cantos, Madrid, Spain., Sanz O; Diseases of the Developing World, GlaxoSmithKline R+D Limited, Tres Cantos, Madrid, Spain., Urones B; Diseases of the Developing World, GlaxoSmithKline R+D Limited, Tres Cantos, Madrid, Spain., Esquivias J; Diseases of the Developing World, GlaxoSmithKline R+D Limited, Tres Cantos, Madrid, Spain., Soni H; Center for Tuberculosis Research, Division of Infectious Diseases, Johns Hopkins Universitygrid.21107.35grid.471401.7grid.21107.35 School of Medicine, Baltimore, Maryland, USA., Tasneen R; Center for Tuberculosis Research, Division of Infectious Diseases, Johns Hopkins Universitygrid.21107.35grid.471401.7grid.21107.35 School of Medicine, Baltimore, Maryland, USA., Tyagi S; Center for Tuberculosis Research, Division of Infectious Diseases, Johns Hopkins Universitygrid.21107.35grid.471401.7grid.21107.35 School of Medicine, Baltimore, Maryland, USA., Li SY; Center for Tuberculosis Research, Division of Infectious Diseases, Johns Hopkins Universitygrid.21107.35grid.471401.7grid.21107.35 School of Medicine, Baltimore, Maryland, USA., Converse PJ; Center for Tuberculosis Research, Division of Infectious Diseases, Johns Hopkins Universitygrid.21107.35grid.471401.7grid.21107.35 School of Medicine, Baltimore, Maryland, USA., Boshoff HI; Tuberculosis Research Section, Laboratory of Clinical Immunology and Microbiology, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, Maryland, USA., Robertson GT; Mycobacteria Research Laboratories, Department of Microbiology, Immunology and Pathology, Colorado State University, Fort Collins, Colorado, USA., Besra GS; Institute of Microbiology and Infection, School of Biosciences, University of Birminghamgrid.6572.6, Birmingham, United Kingdom., Abrahams KA; Institute of Microbiology and Infection, School of Biosciences, University of Birminghamgrid.6572.6, Birmingham, United Kingdom., Upton AM; TB Alliance: Global Alliance for Tuberculosis Drug Development, New York, New York, USA., Mdluli K; TB Alliance: Global Alliance for Tuberculosis Drug Development, New York, New York, USA., Boyle GW; GSK: Research, GlaxoSmithKline R&D, Ware, United Kingdom., Turner S; GSK: Research, GlaxoSmithKline R&D, Ware, United Kingdom., Fotouhi N; TB Alliance: Global Alliance for Tuberculosis Drug Development, New York, New York, USA., Cammack NC; Diseases of the Developing World, GlaxoSmithKline R+D Limited, Tres Cantos, Madrid, Spain., Siles JM; Diseases of the Developing World, GlaxoSmithKline R+D Limited, Tres Cantos, Madrid, Spain., Alonso M; Diseases of the Developing World, GlaxoSmithKline R+D Limited, Tres Cantos, Madrid, Spain., Escribano J; Diseases of the Developing World, GlaxoSmithKline R+D Limited, Tres Cantos, Madrid, Spain., Lelievre J; Diseases of the Developing World, GlaxoSmithKline R+D Limited, Tres Cantos, Madrid, Spain., Rullas-Trincado J; Diseases of the Developing World, GlaxoSmithKline R+D Limited, Tres Cantos, Madrid, Spain., Pérez-Herrán E; Diseases of the Developing World, GlaxoSmithKline R+D Limited, Tres Cantos, Madrid, Spain., Bates RH; Diseases of the Developing World, GlaxoSmithKline R+D Limited, Tres Cantos, Madrid, Spain., Maher-Edwards G; GSK, Brentford, Middlesex, United Kingdom., Barros D; Diseases of the Developing World, GlaxoSmithKline R+D Limited, Tres Cantos, Madrid, Spain., Ballell L; Diseases of the Developing World, GlaxoSmithKline R+D Limited, Tres Cantos, Madrid, Spain., Jiménez E; Diseases of the Developing World, GlaxoSmithKline R+D Limited, Tres Cantos, Madrid, Spain.

Publikováno v: Antimicrobial agents and chemotherapy [Antimicrob Agents Chemother] 2022 Jun 21; Vol. 66 (6), pp. e0013222. Date of Electronic Publication: 2022 May 24.

Two-Way Regulation of MmpL3 Expression Identifies and Validates Inhibitors of MmpL3 Function in Mycobacterium tuberculosis .

Autor: Grover S; Department of Microbiology and Immunology, Weill Cornell Medicine, New York, New York 10065, United States., Engelhart CA; Department of Microbiology and Immunology, Weill Cornell Medicine, New York, New York 10065, United States., Pérez-Herrán E; TB Research Unit, Global Health R&D, GlaxoSmithKline, Severo Ochoa 2, Tres Cantos, Madrid 28760, Spain., Li W; Mycobacteria Research Laboratories, Department of Microbiology, Immunology and Pathology, Colorado State University, Fort Collins, Colorado 80523, United States., Abrahams KA; Institute of Microbiology and Infection, School of Biological Sciences, University of Birmingham, Birmingham B15 2TT, U.K., Papavinasasundaram K; Department of Microbiology and Physiological Systems, University of Massachusetts Medical School, Worcester, Massachusetts 01655, United States., Bean JM; Sloan Kettering Institute, New York, New York 10065, United States., Sassetti CM; Department of Microbiology and Physiological Systems, University of Massachusetts Medical School, Worcester, Massachusetts 01655, United States., Mendoza-Losana A; TB Research Unit, Global Health R&D, GlaxoSmithKline, Severo Ochoa 2, Tres Cantos, Madrid 28760, Spain., Besra GS; Institute of Microbiology and Infection, School of Biological Sciences, University of Birmingham, Birmingham B15 2TT, U.K., Jackson M; Mycobacteria Research Laboratories, Department of Microbiology, Immunology and Pathology, Colorado State University, Fort Collins, Colorado 80523, United States., Schnappinger D; Department of Microbiology and Immunology, Weill Cornell Medicine, New York, New York 10065, United States.

Publikováno v: ACS infectious diseases [ACS Infect Dis] 2021 Jan 08; Vol. 7 (1), pp. 141-152. Date of Electronic Publication: 2020 Dec 15.